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Macrocyclic peptidomimetic beta-secretase (BACE-1) inhibitors with activity in vivo.

Machauer, Rainer, Laumen, Kurt, Veenstra, Siem, Rondeau, Jean-Michel, Tintelnot-Blomley, Marina, Betschart, Claudia, Jaton, Anne-Lise, Desrayaud, Sandrine, Staufenbiel, Matthias, Rabe, Sabine, Paganetti, Paolo and Neumann, Ulf (2009) Macrocyclic peptidomimetic beta-secretase (BACE-1) inhibitors with activity in vivo. Bioorganic & Medicinal Chemistry Letters, 19 (5). pp. 1366-1370. ISSN 1464-3405


The macrocyclic peptidic BACE-1 inhibitors 2a-c show moderate enzymatic and cellular activity. By exchange of the hydroxyethylene- to ethanolamine-transition state mimetic the peptidic character was reduced, providing the highly potent and selective inhibitor 3. Variation of the P' moiety resulted in the macrocyclic inhibitor 14. Both macrocycles show inhibition of BACE-1 in the brain of APP51/16 transgenic mice, 3 (NB-544) after intravenous and 14 (NB-533) after oral application.

Item Type: Article
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Additional Information: Author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used
Keywords: Alzheimer’s disease; BACE-1 inhibition; Macrocycles; Ethanolamine-transition state mimetic; In vivo efficacy in APP51/16 mice
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Date Deposited: 22 Feb 2010 11:50
Last Modified: 31 Jan 2013 00:50


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